Page last updated: 2024-11-08

ilaprazole

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Description

ilaprazole: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID214351
CHEMBL ID2106370
CHEBI ID135544
SCHEMBL ID1179039
MeSH IDM0523237

Synonyms (44)

Synonym
aldenon
ilaprazole
iy-81149
iy 81149
CHEBI:135544
172152-36-2
2-[(4-methoxy-3-methylpyridin-2-yl)methylsulfinyl]-6-pyrrol-1-yl-1h-benzimidazole
iy81149
S3666
776q6xx45j ,
unii-776q6xx45j
ilaprazole [inn]
2-((rs)-((4-methoxy-3-methylpyridin-2-yl)methyl)sulfinyl)-5-(1h-pyrrol-1-yl)-1h-benzimidazole
CHEMBL2106370
noltec
HRRXCXABAPSOCP-UHFFFAOYSA-N
SCHEMBL1179039
ilaprazole [mart.]
ilaprazole [who-dd]
2-(((4-methoxy-3-methylpyridin-2-yl)methyl)sulfinyl)-6-(1h-pyrrol-1-yl)-1h-benzo[d]imidazole
AC-24701
AKOS025401705
CS-6444
HY-101664
AKOS030524778
2-[(4-methoxy-3-methyl-pyridin-2-yl)methylsulfinyl]-6-pyrrol-1-yl-1h-benzoimidazole
DB11964
gtpl10512
FT-0704889
2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1h-pyrrol-1-yl)-1h-benzimidazole
BCP08220
iy81149;iy 81149;ilaprazole
2-[(4-methoxy-3-methylpyridin-2-yl)methylsulfinyl]-5-pyrrol-1-yl-3h-benzoimidazole
2-[(4-methoxy-3-methyl-pyridin-2-yl)methylsulfinyl]-5-pyrrol-1-yl-3h-benzoimidazole
BS-15650
Q15051261
1h-benzimidazole,2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-5-(1h-pyrrol-1-yl)- (9ci)
AMY42072
CCG-268243
2-{[(4-methoxy-3-methylpyridin-2-yl)methyl]sulfinyl}-5-(1h-pyrrol-1-yl)-1h-benzimidazole
iy 81149iy81149
XGA15236
DTXSID10870115
2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1h-pyrrol-1-yl)-1h-benzimidazole; 1h-benzimidazole, 2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-5-(1h-pyrrol-1-yl)- (9ci); 2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1h-pyrrol-1

Research Excerpts

Overview

Ilaprazole (IY-81149) is a new proton-pump inhibitor (PPI) not previously studied in human patients with ulcer disease. It is currently marketed in China and South Korea for the treatment of gastric and duodenal ulcers.

ExcerptReferenceRelevance
"Ilaprazole is a new proton pump inhibitor and is currently marketed in China and South Korea for the treatment of gastric and duodenal ulcer. "( Biotransformation of Ilaprazole in Human Liver Microsomes and Human: Role of CYP3A4 in Ilaprazole Clearance and Drug-Drug Interaction.
Pu, J; Tang, W; Wang, F; Zhu, M, 2018
)
2.24
"Ilaprazole is a kind of benzimidazole proton-pump inhibitor, which was confirmed efficacious and safe in treatment of duodenal ulcer (DU). "( Ilaprazole Compared With Rabeprazole in the Treatment of Duodenal Ulcer: A Randomized, Double-blind, Active-controlled, Multicenter Study.
Fan, L; Haitang, H; Jielai, X; Ling, W; Xianghong, Q; Ying, H, 2019
)
3.4
"Ilaprazole is a novel proton pump inhibitor that has been marketed as an oral therapy for acid-related diseases in China and Korea. "( Intravenous ilaprazole is more potent than oral ilaprazole against gastric lesions in rats.
Gong, ZH; Hou, XM; Hu, HT; Lu, XQ; Su, RB; Xie, HZ; Yu, G, 2014
)
2.22
"Ilaprazole is a highly effective and safe PPI in the treatment of duodenal ulcers. "( Efficacy of ilaprazole in the treatment of duodenal ulcers: a meta-analysis.
Chen, G; Du, JF; Ji, XQ; Yu, B, 2014
)
2.22
"1. Ilaprazole is a novel proton pump inhibitor and this is the first study to investigate the pharmacokinetics, pharmacodynamics and safety of intravenous ilaprazole in healthy volunteers. "( Pharmacokinetics and pharmacodynamics of intravenous ilaprazole in healthy subjects after single ascending doses.
Hu, P; Jiang, J; Lang, L; Ou, N; Shi, R; Wang, H, 2016
)
1.31
"Ilaprazole is a novel proton pump inhibitor that provides effective and long lasting inhibition of intragastric acid secretion. "( Pharmacokinetics, Pharmacodynamics and Safety of Multiple-Infusion Ilaprazole in Healthy Chinese Subjects.
Hu, H; Hu, P; Jiang, J; Lang, L; Ou, N; Shi, R; Wang, H, 2016
)
2.11
"Ilaprazole (IY-81149) is a new proton-pump inhibitor (PPI) not previously studied in human patients with ulcer disease. "( Randomized, parallel, double-blind comparison of the ulcer-healing effects of ilaprazole and omeprazole in the treatment of gastric and duodenal ulcers.
Goh, KL; Ho, KY; Kim, DY; Kuan, A; Mahachai, V; Yoon, HM; Zaño, F, 2009
)
2.02
"Ilaprazole is a new proton pump inhibitor designed for the treatment of gastric ulcers, and limited data is available on the metabolism of the drug. "( Identification of ilaprazole metabolites in human urine by HPLC-ESI-MS/MS and HPLC-NMR experiments.
Chen, Y; Guo, D; Hu, H; Shi, S; Tan, J; Tan, Z; Zhang, W; Zhou, G; Zhou, H, 2010
)
2.14
"Ilaprazole is a new proton pump inhibitor, designed for treatment of gastric ulcers, and developed by Il-Yang Pharmaceutical Co (Seoul, Korea). "( Ilaprazole, a new proton pump inhibitor, is primarily metabolized to ilaprazole sulfone by CYP3A4 and 3A5.
Bae, SK; Kim, DH; Kim, KB; Lee, SJ; Liu, KH; Seo, KA; Shin, JG, 2012
)
3.26

Effects

Ilaprazole (10 mg/day) has a smaller dosage, hence it should be considered more in clinical uses. It has a favorable long half-life and minimal pharmacokinetic variability associated with CYP2C19 polymorphism.

ExcerptReferenceRelevance
"Ilaprazole has a favorable long half-life and minimal pharmacokinetic variability associated with CYP2C19 polymorphism."( Biotransformation of Ilaprazole in Human Liver Microsomes and Human: Role of CYP3A4 in Ilaprazole Clearance and Drug-Drug Interaction.
Pu, J; Tang, W; Wang, F; Zhu, M, 2018
)
1.52
"Ilaprazole (10 mg/day) has a smaller dosage, hence it should be considered more in clinical uses."( A Randomized, Double-blind, Active-Controlled, Multi-center Study of Ilaprazole in the Treatment of Reflux Esophagitis.
Hu, H; Lin, S; Qin, X; Wang, L; Xia, J; Xue, Y; Zhou, L, 2016
)
1.39
"Ilaprazole has a strong effect on intragastric acid control with a dose dependent trend."( [Evaluation of the effect of ilaprazole on intragastric pH in patients with duodenal ulcer].
Hou, XH; Hu, HT; Lin, SR; Qin, XH; Shi, RH; Xia, JL; Yang, YS; Yuan, YZ; Zhang, ST; Zhou, LY, 2010
)
2.09
"Ilaprazole has a favorable long half-life and minimal pharmacokinetic variability associated with CYP2C19 polymorphism."( Biotransformation of Ilaprazole in Human Liver Microsomes and Human: Role of CYP3A4 in Ilaprazole Clearance and Drug-Drug Interaction.
Pu, J; Tang, W; Wang, F; Zhu, M, 2018
)
1.52
"Ilaprazole (10 mg/day) has a smaller dosage, hence it should be considered more in clinical uses."( A Randomized, Double-blind, Active-Controlled, Multi-center Study of Ilaprazole in the Treatment of Reflux Esophagitis.
Hu, H; Lin, S; Qin, X; Wang, L; Xia, J; Xue, Y; Zhou, L, 2016
)
1.39
"Ilaprazole has a strong effect on intragastric acid control with a dose dependent trend."( [Evaluation of the effect of ilaprazole on intragastric pH in patients with duodenal ulcer].
Hou, XH; Hu, HT; Lin, SR; Qin, XH; Shi, RH; Xia, JL; Yang, YS; Yuan, YZ; Zhang, ST; Zhou, LY, 2010
)
2.09

Toxicity

Intravenous ilaprazole was safe and there were no serious adverse events. An unexpectedly high incidence of allergic eye and skin reactions were observed.

ExcerptReferenceRelevance
" Ilaprazole was safe and generally well tolerated; an unexpectedly high incidence of allergic eye and skin reactions were observed but were not specific to any dosing regimen."( The pharmacokinetics, pharmacodynamics and safety of oral doses of ilaprazole 10, 20 and 40 mg and esomeprazole 40 mg in healthy subjects: a randomised, open-label crossover study.
Cho, KH; Kim, DY; Kukulka, M; Lee, JY; Park, HL; Park, SH; Shin, JS; Wu, JT, 2014
)
1.55
" Intravenous ilaprazole was safe and there were no serious adverse events."( Pharmacokinetics, Pharmacodynamics and Safety of Multiple-Infusion Ilaprazole in Healthy Chinese Subjects.
Hu, H; Hu, P; Jiang, J; Lang, L; Ou, N; Shi, R; Wang, H, 2016
)
1.04
" Ilaprazole infusion was safe and well tolerated without serious adverse events."( Efficacy, safety and pharmacokinetics of ilaprazole infusion in healthy subjects and patients with esomeprazole as positive control.
Hou, X; Hu, H; Jiang, J; Liu, F; Liu, X; Ou, N; Qin, X; Shao, F; Wang, H; Xu, W, 2019
)
1.69
" However, the drug is also associated with numerous adverse events."( Predictors of Adverse Events and Determinants of the Voriconazole Trough Concentration in Kidney Transplantation Recipients.
Lin, XB; Peng, FH; Wang, F; Xiang, DX; Xiao, YW; Xie, XB; Xu, P; Yan, M; Zhang, BK; Zhao, YC, 2021
)
0.62
" For the rate of adverse events, there was no significant difference among all the PPIs, vonoprazan, and placebo."( Efficacy and safety of proton pump inhibitors versus vonoprazan in treatment of erosive esophagitis: A PRISMA-compliant systematic review and network meta-analysis.
Chen, J; Deng, W; Xie, Z; Yang, S, 2022
)
0.72

Pharmacokinetics

The H pylori eradication therapy with clarithromycin, amoxicillin and ilaprazole may cause pharmacokinetic interactions. The peak concentration and the area under the concentration-time curve from 0 h to 12 h were significantly decreased, as compared with the single medication group.

ExcerptReferenceRelevance
"To evaluate and compare the pharmacodynamic effects of IY-81149 and omeprazole on gastric pH in patients with gastroesophageal reflux disease."( A comparative pharmacodynamic study of IY-81149 versus omeprazole in patients with gastroesophageal reflux disease.
Boileau, F; Cho, KD; Goldwater, R; Jung, WT; Kim, DY; Lee, SM; Park, DW; Periclou, AP, 2000
)
0.31
" The plasma concentration and pharmacodynamic response were measured in the last dose interval."( Effect of CYP2C19 genetic polymorphism on pharmacokinetics and pharmacodynamics of a new proton pump inhibitor, ilaprazole.
Cho, DY; Cho, H; Cho, M; Choi, MK; Jeong, HE; Kim, DY; Lee, JY; Shin, JG; Shin, JS; Shon, JH; Yeo, CW, 2012
)
0.59
"Following the triple therapy, the peak concentration (C(max)) and the area under the concentration-time curve from 0 h to 12 h (AUC(0→12)) of ilaprazole were significantly decreased, as compared with the single medication group (C(max):1025."( Pharmacokinetic interactions between ilaprazole and clarithromycin following ilaprazole, clarithromycin and amoxicillin triple therapy.
Cao, S; Chen, Y; Fan, L; Guo, D; Hu, HT; Ou-Yang, DS; Qin, XH; Tan, ZR; Wu, HZ; Xiao, K; Zhang, W; Zhou, G; Zhou, HH, 2012
)
0.85
"The H pylori eradication therapy with clarithromycin, amoxicillin and ilaprazole may cause pharmacokinetic interactions that decrease the amount of ilaprazole and its metabolites and elevate that of clarithromycin."( Pharmacokinetic interactions between ilaprazole and clarithromycin following ilaprazole, clarithromycin and amoxicillin triple therapy.
Cao, S; Chen, Y; Fan, L; Guo, D; Hu, HT; Ou-Yang, DS; Qin, XH; Tan, ZR; Wu, HZ; Xiao, K; Zhang, W; Zhou, G; Zhou, HH, 2012
)
0.89
"This review provides an update on the following points: pharmacokinetic profile and metabolism of ilaprazole in relation to its pharmacodynamic properties; comparative data on the pharmacokinetics and pharmacodynamics of ilaprazole with currently available PPIs; and implications for studies on the therapeutic efficacy of ilaprazole in GERD."( The pharmacokinetics of ilaprazole for gastro-esophageal reflux treatment.
Blandizzi, C; de Bortoli, N; Giacchino, M; Marchi, S; Martinucci, I; Savarino, E; Savarino, V, 2013
)
0.91
"Different studies show that ilaprazole, a benzimidazole derivative, has an extended plasma half-life in comparison with all other approved PPIs."( The pharmacokinetics of ilaprazole for gastro-esophageal reflux treatment.
Blandizzi, C; de Bortoli, N; Giacchino, M; Marchi, S; Martinucci, I; Savarino, E; Savarino, V, 2013
)
0.99
"To compare the pharmacodynamic and pharmacokinetic profiles of ilaprazole and esomeprazole."( The pharmacokinetics, pharmacodynamics and safety of oral doses of ilaprazole 10, 20 and 40 mg and esomeprazole 40 mg in healthy subjects: a randomised, open-label crossover study.
Cho, KH; Kim, DY; Kukulka, M; Lee, JY; Park, HL; Park, SH; Shin, JS; Wu, JT, 2014
)
0.88
" The mean steady-state half-life and clearance were comparable to those following single administration."( Pharmacokinetics, Pharmacodynamics and Safety of Multiple-Infusion Ilaprazole in Healthy Chinese Subjects.
Hu, H; Hu, P; Jiang, J; Lang, L; Ou, N; Shi, R; Wang, H, 2016
)
0.67
" The method was successfully applied in pharmacokinetic studies followed by oral administration of GLM and ILA in rats."( Development of Solid-Phase Extraction and HPLC Method for Simultaneous Estimation of Ilaprazole and Glimepiride in Rat Plasma: Application to Pharmacokinetic Studies.
Bakal, RL; Chandewar, AV; Dewani, AP; Mohale, DS; Shelke, PG; Tripathi, AS, 2017
)
0.68
" Ilaprazole has a favorable long half-life and minimal pharmacokinetic variability associated with CYP2C19 polymorphism."( Biotransformation of Ilaprazole in Human Liver Microsomes and Human: Role of CYP3A4 in Ilaprazole Clearance and Drug-Drug Interaction.
Pu, J; Tang, W; Wang, F; Zhu, M, 2018
)
1.71

Compound-Compound Interactions

ExcerptReferenceRelevance
" Consequently, it is predicted that ilaprazole has no significant drug-drug interaction via CYP3A4 inhibition or induction by a coadministered drug."( Biotransformation of Ilaprazole in Human Liver Microsomes and Human: Role of CYP3A4 in Ilaprazole Clearance and Drug-Drug Interaction.
Pu, J; Tang, W; Wang, F; Zhu, M, 2018
)
1.07

Bioavailability

ExcerptReferenceRelevance
" Ilaprazole was not eliminated through urine and the absolute bioavailability was 55."( Pharmacokinetics and pharmacodynamics of intravenous ilaprazole in healthy subjects after single ascending doses.
Hu, P; Jiang, J; Lang, L; Ou, N; Shi, R; Wang, H, 2016
)
1.59

Dosage Studied

The objectives were to investigate the pharmacokinetics, pharmacodynamics and safety of ilaprazole infusion in healthy subjects and patients with esomeprazole as positive control, and then recommend the dosage regimen for Phase 2b/3 studies. The drug was safe and generally well tolerated. An unexpectedly high incidence of allergic eye and skin reactions were observed but were not specific to any dosing regimen.

ExcerptRelevanceReference
" The dose-response relationship for IY-81149 was also evaluated."( A comparative pharmacodynamic study of IY-81149 versus omeprazole in patients with gastroesophageal reflux disease.
Boileau, F; Cho, KD; Goldwater, R; Jung, WT; Kim, DY; Lee, SM; Park, DW; Periclou, AP, 2000
)
0.31
"To investigate the efficacy and safety of a new proton pump inhibitor (PPI), ilaprazole (IY-81149) in the treatment of duodenal ulcers and provide some characteristics of the dose-response relationship for later studies."( A new PPI, ilaprazole compared with omeprazole in the treatment of duodenal ulcer: a randomized double-blind multicenter trial.
Hu, H; Lin, S; Wang, L; Xia, J; Zhou, L, 2011
)
0.99
" Ilaprazole was safe and generally well tolerated; an unexpectedly high incidence of allergic eye and skin reactions were observed but were not specific to any dosing regimen."( The pharmacokinetics, pharmacodynamics and safety of oral doses of ilaprazole 10, 20 and 40 mg and esomeprazole 40 mg in healthy subjects: a randomised, open-label crossover study.
Cho, KH; Kim, DY; Kukulka, M; Lee, JY; Park, HL; Park, SH; Shin, JS; Wu, JT, 2014
)
1.55
"The objectives were to investigate the pharmacokinetics, pharmacodynamics and safety of ilaprazole infusion in healthy subjects and patients with esomeprazole as positive control, and then recommend the dosage regimen for Phase 2b/3 studies."( Efficacy, safety and pharmacokinetics of ilaprazole infusion in healthy subjects and patients with esomeprazole as positive control.
Hou, X; Hu, H; Jiang, J; Liu, F; Liu, X; Ou, N; Qin, X; Shao, F; Wang, H; Xu, W, 2019
)
1
"We developed and validated a simple, convenient and reproducible method for simultaneous estimation of six proton-pump inhibitors (PPIs), omeprazole (OPZ), esomeprazole (EOPZ), lansoprazole (LPZ), pantoprazole (PPZ), rabeprazole (RPZ) and ilaprazole (IPZ) in pharmaceutical dosage forms by a single marker."( Simultaneous Quantitative Analysis of Six Proton-Pump Inhibitors with a Single Marker and Evaluation of Stability of Investigated Drugs in Polypropylene Syringes for Continuous Infusion Use.
Chen, F; Fang, B; He, X; Wang, S, 2020
)
0.74
"The proposed method, which is selective, economical and accurate, was applied successfully for determination of the cited PPIs in their respective pharmaceutical dosage forms."( Simultaneous Quantitative Analysis of Six Proton-Pump Inhibitors with a Single Marker and Evaluation of Stability of Investigated Drugs in Polypropylene Syringes for Continuous Infusion Use.
Chen, F; Fang, B; He, X; Wang, S, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
sulfoxideAn organosulfur compound having the structure R2S=O or R2C=S=O (R =/= H).
benzimidazolesAn organic heterocyclic compound containing a benzene ring fused to an imidazole ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (51)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (1.96)18.2507
2000's6 (11.76)29.6817
2010's33 (64.71)24.3611
2020's11 (21.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 62.73

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index62.73 (24.57)
Research Supply Index4.36 (2.92)
Research Growth Index5.43 (4.65)
Search Engine Demand Index102.05 (26.88)
Search Engine Supply Index2.01 (0.95)

This Compound (62.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials24 (45.28%)5.53%
Reviews6 (11.32%)6.00%
Case Studies0 (0.00%)4.05%
Observational1 (1.89%)0.25%
Other22 (41.51%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]